Tamoxifen derivative-1
Tamoxifen derivative-1 is a derivative of Tamoxifen (HY-13757A) with reduced affinity for estrogen receptor (ER). Tamoxifen derivative-1 blocks estrogen-induced activity, inhibits estrogen-stimulated uterine growth, and exhibits uterotrophic activity in immature rats. Tamoxifen derivative-1 can be used in research related to breast cancer.
For research use only. We do not sell to patients.
- CAS No.: 6462-58-4
- Formula: C28H31NO2
- Molecular Weight:413.55
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
In Vitro
Tamoxifen derivative-1 (Compound 13) binds to estrogen receptors in rat uterus, with a relative affinity of 0.2% that of estradiol[1].
Tamoxifen derivative-1 (48 h) inhibits estradiol-dependent transcriptional activation in HeLa cells via wild-type hERα[2].
Tamoxifen derivative-1 (1000 nM; 48 h) acts as a partial agonist of ERα-dependent transcription in HepG2 cells; the ERαD351A/V mutation abolishes this activity, the ERαD351E mutation increases its activity to the level of tamoxifen, while the ERαD351Y mutation maintains its activity at a moderate level[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Holtzman (immature female, 20-22 days old)[1]
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Dosage:5 μg/day; 15 μg/day; 50 μg/day (antiuterotrophic activity); 50 μg/day (partial estrogen agonist activity)
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Administration:s.c.; daily; 3 days
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Result:Stimulated uterine wet weight to dose-dependent levels, reaching approximately 60 mg at 50 μg/day.
Reduced estradiol-stimulated uterine wet weight from ≈100 mg to approximately 60 mg when co-administered with 1 μg/day estradiol at 50 μg/day.
Had a relative estrogen receptor binding affinity of 0.2% compared to estradiol (set at 100%).
Chemical Information
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CAS No. 6462-58-4
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Molecular Weight 413.55
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Formula C28H31NO2
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SMILES
CC/C(C1=CC=CC=C1)=C(C2=CC=CC=C2)/C3=CC=C(C=C3)OCCN4CCOCC4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. Robertson DW, et al. Antiestrogen basicity--activity relationships: a comparison of the estrogen receptor binding and antiuterotrophic potencies of several analogues of (Z)-1,2-diphenyl-1-[4-[2-(dimethylamino)ethoxy]phenyl]-1-butene (tamoxifen, Nolvadex) having altered basicity. Journal of medicinal chemistry. 1982 Feb;25(2):167-71. [Content Brief]
[2]. Dayan G, et al. Tamoxifen and raloxifene differ in their functional interactions with aspartate 351 of estrogen receptor alpha. Molecular pharmacology. 2006 Aug;70(2):579-88. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Tamoxifen derivative-1 Related Classifications
HY-184725 Related Classifications
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Keywords
- Tamoxifen derivative-1
- 6462-58-4
- Tamoxifen derivative1
- Tamoxifen derivative 1
- Estrogen Receptor/ERR
- Drug Derivative
- HepG2 cells
- estradiol
- rat uterine estrogen receptor
- uterine growth
- human estrogen receptor α
- ERα-dependent transcription
- immature Holtzman rats
- HeLa cells
- breast cancer
- rat estrogen receptor
- Inhibitor
- inhibitor
- inhibit